PEGylated sequence-controlled macromolecules using supramolecular binding to target the Taspase1/Importin α interaction
Autor: | Alexander Höing, Laura Hartmann, Serap Ueclue, Matthias Killa, Shirley K. Knauer, Peter Pasch, Jens Voskuhl |
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Rok vydání: | 2021 |
Předmět: |
Models
Molecular alpha Karyopherins Protein Conformation medicine.medical_treatment Chemie Supramolecular chemistry Sequence (biology) Importin environment and public health Catalysis Polyethylene Glycols Materials Chemistry medicine NLS Receptor Protease Chemistry Metals and Alloys General Chemistry Surfaces Coatings and Films Electronic Optical and Magnetic Materials Ceramics and Composites Biophysics Biologie Nuclear localization sequence Peptide Hydrolases Protein Binding Macromolecule |
Zdroj: | Chemical Communications. 57:3091-3094 |
ISSN: | 1364-548X 1359-7345 |
Popis: | A novel strategy to inhibit the oncologically relevant protease Taspase1 is explored by developing PEGylated macromolecular ligands presenting the supramolecular binding motif guanidiniocarbonylpyrrole (GCP). Taspase1 requires interaction of its nuclear localization signal (NLS) with import receptor Importin α. We show the synthesis and effective interference of PEGylated multivalent macromolecular ligands with Taspase1-Importin α-complex formation. |
Databáze: | OpenAIRE |
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